Pyridinone derivatives: Specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity

Proceedings of the National Academy of Sciences of the United States of America

Volumn 88, Issue 15, 1991, Pages 6863-6867

  Goldman, Mark E ^a   Nunberg, Jack H ^a   O'Brien, Julie A ^a   Quintero, Julio C ^a   Schleif, William A ^a   Freund, Kurt F ^a   Gaul, S Lee ^a   Saari, Walfred S ^a   Wai, John S ^a   Hoffman, Jacob M ^a   Anderson, Paul S ^a   Hupe, Donald J ^a   Emini, Emilio A ^a   Stern, Andrew M ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Acquired immunodeficiency syndrome; Antiviral agents; Inhibition kinetics; Synergy

Indexed keywords

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

3 [(4,7 DICHLORO 2 BENZOXAZOLYLMETHYL)AMINO] 5 ETHYL 6 METHYL 2(1H) PYRIDONE; 3 [(4,7 DIMETHYL 2 BENZOXAZOLYLMETHYL)AMINO] 5 ETHYL 6 METHYL 2(1H) PYRIDONE; 3 [[(4,7 DICHLORO 2 BENZOXAZOLYL)METHYL]AMINO] 5 ETHYL 6 METHYL 2(1H) PYRIDONE; 3 [[(4,7 DIMETHYL 2 BENZOXAZOLYL)METHYL]AMINO] 5 ETHYL 6 METHYL 2(1H) PYRIDONE; 4,5,6,7 TETRAHYDRO 5 METHYL 6 (3 METHYL 2 BUTENYL)IMIDAZO[4,5,1 JK][1,4]BENZODIAZEPINE 2(1H) THIONE; DIDANOSINE; ENZYME INHIBITOR; NEVIRAPINE; PYRIDINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE; UNCLASSIFIED DRUG; ZIDOVUDINE;

ANTIVIRAL ACTIVITY; ARTICLE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; PRIORITY JOURNAL; T LYMPHOCYTE;

ANTIVIRAL AGENTS; CELL LINE; HIV; HIV-1; HUMAN; INDICATORS AND REAGENTS; KINETICS; PYRIDONES; REVERSE TRANSCRIPTASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; VIRUS REPLICATION;

EID: 0026003110     PISSN: 00278424     EISSN: None     Source Type: Journal    
DOI: 10.1073/pnas.88.15.6863     Document Type: Article

References (27)

1. Fischl, M. A., Richman, D. D., Grieco, M. H., Gottlieb, M. S., Volberding, P. A., Laskin, O. L., Leedom, J. M., Groopman, J. E., Mildvan, D., Schooley, R. T., Jackson, G. G., Durack, D. T., King, D. & the AZT Collaborative Working Group (1987) N. Engl. J. Med. 317, 185-191.
2. Butler, K. M., Husson, R. N., Balis, F. M., Brouwers, P., Eddie, J., El-Amin, D., Gress, J., Hawkins, P., Jarosinski, P., Moss, H., Poplack, D., Santacroce, S., Venzon, D., Wiener, L., Wolters, P. & Pizzo, P. A. (1991) N. Engl. J. Med. 324, 137-144.
3. Mitsuya, H., Yarchoan, R. & Broder, S. (1990) Science 249, 1533-1542.
4. Yarchoan, R. & Broder, S. (1989) Pharmacol. Ther. 40, 329-348.
5. Larder, B. A., Darby, G. & Richman, D. D. (1989) Science 243, 1731-1734.
6. Azzolina, B., Behrens, N. D., Chang, B., Dahlgren, M. E., George, H., Menke, J. T., Linemeyer, D. L. & Hupe, D. J. (1990) FASEB J. 4, A2253.
7. Goldman, M. E., Salituro, G. S., Bowen, J. A., Williamson, J. M., Zink, D. L., Schleif, W. A. & Emini, E. A. (1990) Mol. Pharmacol. 38, 20-25.
8. Goff, S., Traktman, P. & Baltimore, D. (1981) J. Virol. 38, 239-248.
9. Chang, L. M. S., Rafter, E., Augl, C. & Bollum, F. J. (1984) J. Biol. Chem. 259, 14679-14687.
10. Starnes, M. C. & Cheng, Y. (1989) J. Biol. Chem. 264, 7073-7077.
11. Popovic, M., Sarnagadharan, M. G., Read, E. & Gallo, R. C. (1984) Science 224, 497-500.
12. Gallo, R. C., Salahuddin, S. Z. & Popovic, M. (1984) Science 224, 500-503.
13. Miyoshi, I., Kibonishi, I., Yoshimoto, S., Akagi, T., Ohtsuki, Y., Shiraishi, Y., Nagata, K. & Himura, Y. (1981) Nature (London) 294, 770-771.
14. Gurgo, C. H., Guo, H.-G., Franchini, G., Aldovini, A., Collalti, E., Farrell, K., Wong-Staal, F., Gallo, R. C. & Reitz, M. S. (1988) Virology 164, 531-536.
15. Katzenstein, D. A., Vujcic, L. K., Latif, A., Boulos, R., Halsey, N. A., Quinn, T. C., Rastogi, S. C. & Quinnan, G. V. (1990) J. Acquired Immune Defic. Syndr. 3, 810-816.
16. Hahn, B. H., Shaw, G. M., Taylor, M. E., Redfield, R. R., Markham, P. D., Salahuddin, S. Z., Wong-Staal, F., Gallo, R. C., Parks, E. S. & Parks, W. P. (1986) Science 232, 1548-1553.
17. Hahn, B. H., Shaw, G. M., Arya, S. K., Popovic, M., Gallo, R. C. & Wong-Staal, F. (1984) Nature (London) 312, 166-169.
18. Foley, G. E. (1965) Cancer 18, 522-529.
19. Elion, G. B., Sivger, S. & Hitchings, G. B. (1954) J. Biol. Chem. 208, 477-488.
20. Chou, T. C. & Talalay, P. (1987) in New Avenues in Developmental Cancer Chemotherapy, eds. Harrap, K. R. & Connors, T. A. (Academic, Orlando, FL), pp. 37-64.
21. Morrison, J. F. (1982) Trends Biochem. Sci. 7, 102-105.
22. Cha, S. (1975) Biochem. Pharmacol. 24, 2177-2185.
23. Hardewign, P., Balzarini, J., De Clercq, E., Pauwels, R., Baba, M., Broder, S. & Vanderhaghe, H. (1987) J. Med. Chem. 30, 1270-1278.
24. Pauwels, R., Andries, K., Desmyter, J., Schols, D., Kukla, M. J., Breslin, H. J., Raeymaeckers, A., Van Gelder, J., Woestenborghs, R., Heykants, J., Schellekins, K., Janssen, M. A. C., De Clercq, E. & Janssen, P. A. J. (1990) Nature (London) 343, 470-474.
25. Merluzzi, V. J., Hargrave, K. D., Labodia, M., Grozinger, K., Skoog, M., Wu, J. C., Shih, C.-K., Eckner, K., Hattox, S., Adams, J., Rosenthal, A. S., Faanes, R., Eckner, R. J., Koup, R. A. & Sullivan, J. L. (1990) Science 250, 1411-1413.
26. Debyser, Z., Pauwels, R., Andries, K., Desmyter, J., Kukla, M., Janssen, P. A. J. & De Clercq, E. (1991) Proc. Natl. Acad. Sci. USA 88, 1451-1455.
27. Nunberg, J. H., Schleif, W. A., Boots, E. J., O'Brien, J. A., Quintero, J. C., Hoffman, J. M., Emini, E. A. & Goldman, M. E. (1991) J. Virol. 65, in press.